Biological Information

Background Information:

Cholecystokinin receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Cholecystokinin CCK2 receptors are widely distributed in the brain, with highest concentrations in the striatum, cerebral cortex and limbic system, but can also be found in the stomach.

Family:

GPCR

Sub Family:

Cholecystokinin

Class:

Class A

Protein Name:

CCK2 (CCKB)

Uniprot Number:

P32239

Protein Aliases:

CCK-BR|Cholecystokinin-2 receptor|CCK2-R

Gene Name:

CCKBR

Gene ID:

887

Gene Aliases:

CCKRB

Accession Number:

NM_176875

Organism:

Human

Construct Details:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at 37°C

Control Inhibitor:

YM022

Control Activator:

CCK-8s (10 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL testing. 2) Dose Response: 90 µL of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

3960

Name

Lorglumide

Measurement

8800nM - IC50

PubChem ID

122130

Name

YM022

Measurement

0.66nM - IC50

PubChem ID

4355450

Name

133040-77-4

Measurement

4400nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Cholecystokinin CCK2 receptor agonism may enhance anxiety and gastric acid secretion while receptor antagonism may impair memory.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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